Biorelevant dissolution models to assess precipitation of weak base drug
Penulis/Author
VIVIANE ANNISA (1); Prof. Dr. Teuku Nanda Saifullah Sulaiman, S.Si., M.Si., Apt. (2); Prof. Dr. apt. Agung Endro Nugroho, S.Si., M.Si. (3)
Tanggal/Date
21 2020
Kata Kunci/Keyword
Abstrak/Abstract
The impact of precipitation can affect the amount of drug absorbed, therebyaffecting the amount of drug in the systemic body. The precipitation processis preceded by a supersaturation phase, caused by decreased drug solubilityin the gastrointestinal tract. This precipitation occurs for weak base drugswith low solubility. When the drug entering the small intestine, the solubil-ity of weak base drugs decrease, then occurs supersaturation, which leads toprecipitation, so that drug precipitation is one of a challenge for the pharma-ceutical industry in drug development. Precipitation testing of water-solubleweak base drugs can be carried out by the pH shift method to describe the gas-trointestinal pH gradient from gastric to small intestine. This pH change cancause supersaturation and then trigger precipitation, especially for weak basedrugs. The methods that can used to assess precipitation drug is modi?icationof the USP dissolution which are two compartment and multi compartmentmodel. The choice of dissolution medium play an important role in the testresults. The use of bio relevant medium can produce closer in vitro and invivo correlations than the use of buffers. Generally, the medium used to sim-ulate the weakly condition in the small intestine is FaSSIF (Fasted State Simu-latedIntestinalFluid)orFeSSIF(FedStateStimulateIntestinalFluid)medium.The medium used to simulate the acidic condition in the stomach is FaSSGF(Fasted state simulated gastric ?luid) or FeSSGF (Fed state simulated gastric?luid) medium.
